Colletofragarone A2 and Colletoins A-C from a Fungus <i>Colletotrichum</i> sp. Decrease Mutant p53 Levels in Cells.

Basic Information

ID: ALA4840377

Journal: J Nat Prod

Title: Colletofragarone A2 and Colletoins A-C from a Fungus Colletotrichum sp. Decrease Mutant p53 Levels in Cells.

Authors: Sadahiro Y, Hitora Y, Tsukamoto S.

Abstract: p53 is frequently mutated in tumor cells. Mutant p53 (mut p53) accumulates in cells to promote cancer progression, invasion, and metastasis, and it is attracting attention as a target for cancer therapies. In this study, we used immunofluorescence staining of Saos-2 cells harboring doxycycline-inducible p53^R175H [Saos-2 (p53^R175H) cells] to search for compounds from natural sources that can target mut p53 and found an extract of Colletotrichum sp. (13S020) that was active. Bioassay-guided fractionation of the extract afforded a known polyketide, colletofragarone A2 (1), and three new analogues, colletoins A-C (2-4). The relative and absolute configurations of 1 were determined by the spectroscopic method and DFT calculation. Compounds 1 and 2 inhibited the growth of Saos-2 (p53^R175H) cells and decreased mut p53 in the cells.

CiteXplore: 34854682

DOI: 10.1021/acs.jnatprod.1c00913

Patent ID: ┄

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